Effectivness of certain 2nd generation ALK inhibitors against specific ALK mutations

Four 2nd generation ALK inhibitors (Ceritinib, Alectinib, AP26113, and ASP3026) were tested in vitro against six known mutations of the ALK fusion gene.

Generally, AP26113 (brigatinib) was most effective and ASP3026 was least effective. In some cases one drug worked against one mutation while another drug worked against a different mutation.

The mutation G1202R was resistant to all four of the 2nd generation ALK inhibitors (least resistantance developed for AP26113 (brigatinib)).

http://onlinelibrary.wiley.com/enhanced/doi/10.1002/cam4.413

This entry was posted in alectinib - Alecensa from Chugai - Roche - GenenTech, AP26113 - brigatinib from Ariad, ASP3026 from Astellas, ceritinib - Zykadia from Novartis, Lung cancer, Research, Resistance to treatment. Bookmark the permalink.

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